Drug intelligence / Profile preview

linagliptin + metformin + sulphonylurea

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Small Molecules
Administration
Oral
01

Overview

**linagliptin + metformin + sulphonylurea** is a triple oral combination therapy for type 2 diabetes mellitus. This regimen combines three distinct antihyperglycemic agents: *linagliptin* (a dipeptidyl peptidase-4 inhibitor), *metformin* (a biguanide), and a *sulphonylurea* (e.g., glimepiride, glibenclamide, or other drugs in this class). - **Mechanism of action:** - Linagliptin inhibits dipeptidyl peptidase-4, increasing incretin levels and thus enhancing glucose-dependent insulin secretion and suppressing glucagon secretion. - Metformin primarily inhibits hepatic gluconeogenesis and reduces intestinal glucose absorption, while increasing insulin sensitivity. - Sulphonylureas stimulate pancreatic beta-cell insulin secretion by inhibiting ATP-sensitive potassium channels. These agents act via complementary mechanisms to improve glycemic control when used together, especially in patients whose diabetes is not adequately controlled by dual therapy. - **Indication:** Used to improve glycemic control in adults with type 2 diabetes mellitus, as an adjunct to diet and exercise, when dual therapy is insufficient[1][2][3]. - **Common sulphonylureas** included in studies are glimepiride and glibenclamide[3]. - **Safety:** The most common adverse effect is hypoglycemia (particularly from the sulphonylurea component), and others include gastrointestinal upset (from metformin)[2][3]. - **Approved in the EU/US** for the above indication as a triple combination, but not as a fixed-dose triple pill; used as a regimen consisting of individual drugs (or fixed linagliptin+metformin with sulphonylurea added separately)[2][3].

02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)ND1 (Mitochondrial electron transport chain complex I)KATP channel (ATP-sensitive potassium channel)

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